Assay Systems for HIV-1 Proteinase and Their Use for Evaluation of Inhibitors

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Billich A. Hammerschmid F. , and Winkler G. (1990) Purification, assay and kinetic features of HIV-1 proteinase. Biol Chem Hoppe-Seyler 371: 265–272.

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Cheng Y.S.E. McGowan M.H. Kettner C.A. Schloss J.V. Erickson-Viitanen S. , and Yin F.H. (1990) High-level synthesis of recombinant HIV-1 protease and the recovery of active enzyme from inclusion bodies. Gene 87: 243–248.

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Darke P.L. Nutt R.F. Brady S.F. Garsky V.M. Ciccarone T.M. Leu C.T. Lumma P.K. Freidinger R.M. Veber D.F. , and Sigal I.S. (1988) HIV-1 protease specificity of peptide cleavage is sufficient for processing of gag and pol polypeptides. Biochem Biophys Res Commun 156: 297–303.

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Geoghegan K.F. Spencer R.W. Danley D.E. Contillo L.G. , and Andrews G.C. (1990) Fluorescence-based continuous assay for the aspartyl protease of human immunodeficiency virus-1. FEBS Lett 262: 119–122.

Gheysen D. Jacobs E. de Foresta F. Thiriart C. Francotte M. Thines D. , and De Wilde M. (1989) Assembly and release of HIV-1 precursor Pr55^gag virus-like particles from recombinant baculovirus-infected insect cells. Cell 59: 103–112.

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Gowda S.D. Stein B.S. , and Engleman E.G. (1989a) Identification of protein intermediates in the processing of the p55 HIV-1 gag precursor in cells infected with recombinant vaccinia virus. J Biol Chem 264: 8459–8462.

Gowda S.D. Stein B.S. Steimer K.S. , and Engleman E.G. (1989b) Expression and processing of human immunodeficiency virus type 1 gag and pol genes by cells infected with a recombinant vaccinia virus. J Virol 63: 1451–1454.

Graves M.C. Meidel M.C. Pan Y.C.E. Manneberg M. Lahn H.W. , and Grüninger-Leitch F. (1990) Identification of a human immunodeficiency virus-1 protease cleavage site within the 66,000 dalton subunit of reverse transcriptase. Biochem Biophys Res Commun 168: 30–36.

Grinde B. Hungnes O. , and Tjøtta E. (1989) The proteinase inhibitor pepstatin A inhibits formation of reverse transcriptase in H9 cells infected with human immunodeficiency virus 1. AIDS Res Human Retrovir 5: 269–274.

Hansen J. Billich S. Schulze T. Sukrow S. , and Mölling K. (1988) Partial purification and substrate analysis of bacterially expressed HIV protease by means of monoclonal antibody. EMBO J 7: 1785–1791.

Heimbach J.C. Garsky V.M. Michelson S.R. Dixon R.A.F. Sigal I.S. , and Darke P.L. (1989) Affinity purification of the HIV-1 protease. Biochem Biophys Res Commun 164: 955–960.

Hirel Ph.H. Parker F. Boizeau J. Jung G. Outerovitch D. Dugué A. Peltiers C. Giuliacci C. Boulay R. Levievre Y. Cambou B. Mayaux J.F. , and Cartwright T. (1990) HIV-1 aspartic proteinase: high-level production and automated fluorometric screening assay of inhibitors. Antiviral Chem Chemother 1: 9–15.

Hostomsky Z. Appelt K. , and Ogden R.C. (1989) High-level expression of self-processed HIV-1 protease in Escherichia coli using a synthetic gene. Biochem Biophys Res Commun 161: 1056–1063.

Jacobs E. Gheysen D. Thines D. Francotte M. , and De Wilde M. (1989) The HIV-1 gag precursor Pr55^gag synthesized in yeast is myristoylated and targeted to the plasma membrane. Gene 79: 71–81.

Katoh I. Ikawa Y. , and Yoshinaka Y. (1989) Retrovirus protease characterized as a dimeric aspartic proteinase. J Virol 63: 2226–2232.

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Kempf D.J. Norbeck D.W. Codacovi L.M. Wang X.C. Kohlbrenner W.E. Wideburg N.E. Paul D.A. Knigge M.F. Vasavanonda S. Craig-Kennard A. Saldivar A. Rosenbrook W. Jr Clement J.J. Plattner J.J. , and Erickson J. (1990) Structure-based, C₂ symmetric inhibitors of HIV protease. J Med Chem 33: 2687–2689.

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Konvalinka J. Strop S. Velek J. Cerna V. Kostka V. Phylip L.H. Richards A.D. Dunn B.M. , and Kay J. (1990) Sub-site preferences of the aspartic proteinase from the human immunodeficiency virus, HIV-1. FEBS Lett 268: 35–38.

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Kräusslich H.G. Schneider H. Zybarth G. Carter C.A. , and Wimmer E. (1988) Processing of in vitro-synthesized gag precursor proteins of human immunodeficiency virus (HIV) type 1 by HIV proteinase generated in Escherichia coli. J Virol 62: 4393–4397.

Lapatto R. Blundell T. Hemmings A. Overington J. Wilderspin A. Wood S. Merson J.R. Whittle P.J. Danley D.E. Geoghegan K.F. Hawrylik S.J. Lee S.E. Scheld K.G. , and Hobart P.M. (1989) X-ray analysis of HIV-1 proteinase at 2.7 A resolution confirms structural homology among retroviral enzymes. Nature 342: 299–302.

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Loeb D.D. Swanstrom R. Everitt L. Manchester M. Stamper S.E. , and Hutchison C.A. III (1989b) Complete mutagenesis of the HIV-1 protease. Nature 340: 397–400.

McKeever B.M. Navia M.A. Fitzgerald P.M.D. Springer J.P. Leu C.T. Heimbach J.C. Herber W.K. Sigal I.S. , and Darke P.L. (1989) Crystallization of the aspartylprotease from the human immunodeficiency virus, HIV-1. J Biol Chem 264: 1919–1921.

McQuade T.J. Tomaselli A.G. Liu L. Karacostas V. Moss B. Sawyer T.K. Heinrikson R.L. , and Tarpley W.G. (1990) A synthetic HIV-1 protease inhibitor with antiviral activity arrests HIV-like particle maturation. Science 247: 454–457.

Madisen L. Travis B. Hu S.L. , and Purchio A.F. (1987) Expression of the human immunodeficiency virus gag gene in insect cells. Virology 158: 248–250.

Margolin N. Heath W. Osborne E. Lai M. , and Vlahos C. (1990) Substitutions at the P₂′ site of gag P17-P24 affect cleavage efficiency by HIV-1 protease. Biochem Biophys Res Commun 167: 554–560.

Matayoshi E.D. Wang G.T. Krafft G.A. , and Erickson J. (1990) Novel fluorogenic substrates for assaying retroviral proteases by resonance energy transfer. Science 247: 954–958.

Meek T.D. Dayton B.D. Metcalf B.W. Dreyer G.B. Strickler J.E. Gorniak J.G. Rosenberg M. Moore M.L. Magaard V.W. , and Debouck C. (1989) Human immunodeficiency virus 1 protease expressed in Escherichia coli behaves as a dimeric aspartic protease. Proc Natl Acad Sci USA 86: 1841–1845.

Meek T.D. Lambert D.M. Dreyer G.B. Carr T.J. Tomaszek T.A. Jr Moore M.L. Strickler J.E. Debouck C. Hyland L.J. Matthews T.J. Metcalf B.W. , and Petteway S.R. (1990) Inhibition of HIV-1 protease in infected T-lymphocytes by synthetic peptide analogues. Nature 343: 90–92.

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Moore M.L. Bryan W.M. Fakhoury S.A. Magaard V.W. Huffman W.F. Dayton B.D. Meek T.D. Hyland L. Dreyer G.B. Metcalf B.W. Strickler J.E. Gorniak J.G. , and Debouck C. (1989) Peptide substrates and inhibitors of the HIV-1 protease. Biochem Biophys Res Commun 159: 420–425.

Nashed N.T. Louis J.M. Sayer J.M. Wondrak E.M. Mora P.T. Oroszlan S. , and Jerina D.M. (1989) Continuous spectrophotometric assay for retroviral proteases of HIV-1 and AMV. Biochem Biophys Res Commun 163: 1079–1085.

Nutt R.F. Brady S.F. Darke P.L. Ciccarone T.M. Colton C.D. Nutt E.M. Rodkey J.A. Bennett C.D. Waxman L.H. Sigal I.S. Anderson P.S. , and Veber D.F. (1988) Chemical synthesis and enzymatic activity of a 99-residue peptide with a sequence proposed for the human immunodeficiency virus protease. Proc Natl Acad Sci USA 85: 7129–7133.

Overton H.A. Fujii Y. Price I.R. , and Jones I.M. (1989) The protease and gag gene products of the human immunodeficiency virus: Authentic cleavage and post-translational modification in an insect cell expression system. Virology 170: 107–116.

Pauwels R. Balzarini J. Baba M. Snoeck R. Schols D. Herdwijn P. Desmyter J. , and De Clerq E. (1988) Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds. J Virol Meth 20: 309–321.

Phylip L.H. Richards A.D. Kay J. Konvalinka J. Strop P. Blaha I. Velek J. Kostka V. Ritchie A.J. Broadhurst A.V. Farmerie W.G. Scarborough P.E. , and Dunn B.M. (1990) Hydrolysis of synthetic chromogenic substrates by HIV-1 and HIV-2 proteinases. Biochem Biophys Res Commun 17: 439–443.

Pichuantes S. Babé L.M. Barr P.J. , and Craik C.S. (1989) Recombinant HIV 1 protease secreted by Saccharomyces cerevisiae correctly processes myristylated gag polyprotein. Proteins Struct Funct Genet 6: 324–337.

Rich D.H. Green J. Toth M.V. Marshall G.R. , and Kent S.B.H. (1990) Hydroxyethylamine analogues of the p17/p24 substrate cleavage site are tight-binding inhibitors of HIV protease. J Am Chem Soc 33: 1285–1288.

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Richards A. Phylip L.H. Farmerie W.G. Scarborough P.E. Alvarez A. Dunn B.M. Hirel P.H. Konvalinka J. Strop P. Pavlickova L. Kostka V. , and Kay J. (1990) Sensitive, soluble chromogenic substrates for HIV-1 proteinase. J Biol Chem 265: 7733–7736.

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Shoeman R.L. Young D. Pottathil R. Victor J. Conroy R.R. Crowl R.M. Coleman T. Heimer E. Laci C.Y. Ganguly K. Reddy E.P. Skalka A.M. Pine P.R. Khan F.R. , and Weissbach H. (1987) Comparison of recombinant human immunodeficiency virus gag precursor and gag/env fusion proteins and a synthetic env peptide as diagnostic reagents. Anal Biochem 161: 370–379.

Shoeman R.L. Höner B. Stoller T.J. Kesselmeier C. Miedel M.C. Traub P. , and Graves M.C. (1990a) Human immunodeficiency virus type 1 protease cleaves the intermediate filament proteins vimentin, desmin, and glial fibrillary acidic protein. Proc Natl Acad Sci USA 87: 6336–6340.

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